1-(3-(2-(1-Benzothiophen-5-yl)ethoxy)propyl)azetidin-3-ol (hereinafter referred to as “Compound A”) or a salt thereof is a compound having neuroprotective, nerve regeneration-promoting and neurite outgrowth effects, and useful as a therapeutic agent for central and peripheral neurological diseases (Patent Document 1).
Compound A or a salt thereof is orally administered. Thus, there is a need for an oral formulation comprising Compound A or a salt thereof. The most preferred dosage form in general is a tablet (Non-Patent Document 1). However, Compound A or a salt thereof has properties such as low compression moldability, proneness to a tableting trouble (sticking), and insufficient preservation stability at high humidity.
In producing tablets, a mixed powder for tableting is required to have compression moldability. Low compression moldability of the mixed powder for tableting decreases the hardness of tablets. In this case, there is a fear of damage of tablets in packaging or transportation or abrasion or chipping of tablets in a coating machine in film-coating of the tablets.
The method, which involves blending a highly moldable excipient such as crystalline cellulose to produce a mixed powder for tableting having a high compression moldability to produce tablets having necessary hardness (Non-Patent Document 2), has been reported (Non-Patent Document 3).
The tablet or the like, which contains Compound A or a salt thereof, lactose, crystalline cellulose and a diluent, is known (Patent Document 2), however, there is a need for improvements in dissolvability and stability under preservation conditions of heating and moisturizing.